Applying internal Mannich reaction on N'-(substituted benzoyl)-2-(methyl- amino) benzohydrazide (IIa-h), under different conditions, afforded a new series of 2, 3-dihydroquinazolin-4(1H)-one derivatives (IIIa-g). The carbohydrazide; N'-(p-chlorobenzoyl)-2-(methyl- amino) benzohydrazide (IIe) is the only exception which gives benzotriazepin- 5(2H)-one. All carbohydrazides (IV) were prepared by condensing N-methylisatoic anhydride with substituted benzoic acid hydrazides. The obtained 2, 3-dihydroquinazolin-4(1H)-one derivatives (IIIa-g) were subjected to biological screening as analgesic and anti-inflammatory. The quinazolinone (IIIb, IIIg) showed higher analgesic activity over celecoxib while (IIIg) is more active than diclophenac sodium as anti-inflammatory.
Samy M. Ibrahim*, M. Abo-Kul, Moustafa K. Soltanand Ahmed S. Helal.
Clotrimazole is an antifungal agent widely used as a first line treatment for oral candidiasis. Clotrimazole is a poorly water soluble drug, so solubility is main constraints for its oral bioavailability. An attempt has been made to increase its solubility by complexation with β‐cyclodextrin and then formulating mucoadhesive tablets of best formulation with β‐cyclodextrin. The phase solubility analysis indicated the formation of 1:1 molar inclusion complexes. The inclusion complexes prepared by different methods viz. Physical mixture, Kneading and Solvent evaporation methods. The prepared complexes were characterized using DSC. Mucoadhesive tablet formulations were prepared by direct compression technique using four mucoadhesive polymers namely Carbopol 974P, HPMC K15M and HPMC K4M. The entire formulation blend was evaluated Precompression studies and prepared mucoadhesive tablets were evaluated for post compression studies and the results were found to be within the limits. The compatibility studies were performed which resulted in no interactions between drug and excipients.
Naga Prasad Arepalliy*, Malleswara Rao Pillaboina, K. Navya Sree, K. L. N. Mallikharjunarao, K. V. V. S. Ujwala, M. Manjula.
A new series of 2-hydrazino-quinazolinone (III) and 3-amino-triazolo-quinazolinones (VIIa-g) were prepared upon hydrazinolysis of 2-mercapto-quinazolinone intermediates (II,VIa-g) respectively. These compounds were condensed with aromatic aldehydes, for its confirmation; where compound (III) gives rise 2-(2-substitutedarylidenehydrazinyl)-3-(phenylamino) quinazolin-4(3H)-one (IVa-f) and compound (VIIa) gives rise 3-(4-chloro benzylideneamino)-2-phenyl-[1,2,4] triazolo[5,1-b]quinazolin-9(3H)-one (X). The biological testing of the target compounds (IVe, IVf, VIIa,VIIf) showed moderate anti-inflammatory activity with low ulcerogenic index compared with diclofenac sodium and celecoxib.
Samy M. Ibrahim*, M. Abo-Kul, Moustafa K. Soltan, Ahmed S. Helal.
A simple, precise, rapid, and reproducible reverse phase liquid chromatographic method developed and validated for the quantification of Paliperidone in bulk drug and in Pharmaceutical dosage form. Separation was achieved under optimized chromatographic condition on a PhenomenaxLunaC18 (ODS) column (150 X 4.6 mm i.d., particle size 5m). The mobile phase consisting of phosphate buffer pH 3.0: Acetonitrile (60:40, v/v). An isocratic elution was achieved at a flow rate of 1 ml/ min at ambient temperature. The detection was carried out at 225nm using Shimadzu UV-Visible detector SpD-10AVP. The retention time of Paliperidone was found to be 5.02 min. The calibration curve was linear in the concentration range of 5-30mg/ ml (r2═ 0.9999).The limit of detection and the limit of quantification were found to be 0.580531 mg/ml and 1.75918mg/ml respectively. The amount of Paliperidone present in the formulation was found to be 99.79 ±0.8075. The method was validated statistically using the SD, % RSD and SE and the values were found to be within the limits. The recovery studies were performed and the percentage recoveries were found to be 101.10±1.635%. So, the proposed method was found to be simple, specific, linear, and rugged. Hence it can be applied for routine analysis of Paliperidone in the Pharmaceutical formulation.